ANALOGS OF MONENSIN WITH A MODIFIED C-25-C-26 MOIETY - NA+/K+ SELECTIVITY AND BIOLOGICAL-ACTIVITY
ANALOGS OF MONENSIN WITH A MODIFIED C-25-C-26 MOIETY - NA+/K+ SELECTIVITY AND BIOLOGICAL-ACTIVITY
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DOI：
10.1080/00021369.1990.10870088
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发表时间：
1990-05-01
期刊：
影响因子：
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通讯作者：
JEMINET, G
中科院分区：
文献类型：
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作者：
GABOYARD, C;DAUPHIN, G;JEMINET, G
制备了莫能菌素（1）的C25-C26化学衍生物：25-去羟甲基，25-氧代（2）; 25，26-亚异丙基（3）; 25-O-甲基（4）; 26-O-酰基（5）; 26-O-[N-氯苯基]氨基甲酰基（6）;和26-O-[N-氯苯基，N-甲基]氨基甲酰基（7）。通过这些类似物在水/甲苯-丁醇（70：30）体系中的Na+和K+萃取的测量显示C[26]H2-OH臂对于由莫能菌素形成的1：1复合物的稳定性和选择性的关键作用。测定了与Na+/K+阳离子亲和力相关的小鼠抗生素活性和毒性。
C25-C26 chemical derivatives of monensin (1) were prepared: 25-dehydroxymethyl, 25-oxo (2); 25,26-isopropyliden (3); 25-O-methyl (4); 26-O-acyl (5); 26-O-[N-chlorophenyl]carbamoyl (6); and 26-O-[N-chlorophenyl, N-methyl]carbamoyl (7). Measurements of Na+ and K+ extractions in a water/toluene-butanol (70:30) system by these analogs showed the key role of the C[26]H2-OH arm for the stability and selectivity of 1:1 complexes formed by monensin. The antibiotic activity and toxicity in mice were determined in relation to the Na+/K+ cationic affinity.